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Pharmacokinetics: Drug–Drug Interactions01:25

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Drug interactions occur when the pharmacological effect of one drug is altered by another substance, either enhancing or diminishing its activity. The drug whose activity is altered is known as the object drug, and the substance causing the alteration is called the agent drug or the precipitant. The net effects of these interactions are mostly undesirable, leading to decreased effectiveness or increased adverse effects. In rare cases, interactions can be beneficial, such as the enhanced...
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Post-approval, manufacturers may modify an approved new or generic drug product. Such modifications can encompass alterations in the Active Pharmaceutical Ingredient (API), manufacturing process, formulation, batch size, manufacturing site, and container closure system (FDA Guidance for Industry, April 2004). Often, a drug product may undergo multiple changes.These modifications require careful evaluation to determine their potential impact on the drug product's identity, strength, quality,...
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A drug interaction occurs when the concurrent use of another drug, food, or an external substance alters the pharmacological activity of a drug. This interaction can modify the action of the original drug, affecting its effectiveness and safety.Drug–food interactions are significant as they impact drug absorption, metabolism, and excretion. For example, grapefruit juice is a well-known disruptor of drug metabolism. It inhibits the cytochrome P450 3A4 enzyme, crucial for the metabolism of...
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N-Acylhydrazones as drugs.

Sreekanth Thota1, Daniel A Rodrigues2, Pedro de Sena Murteira Pinheiro2

  • 1National Institute for Science and Technology on Innovation on Neglected Diseases (INCT/IDN), Center for Technological Development in Health (CDTS), Fundação Oswaldo Cruz - Ministério da Saúde, Av. Brazil 4036 - Prédio da Expansão, 8° Andar - Sala 814, Manguinhos, 21040-361 Rio de Janeiro, RJ, Brazil; Laboratório de Avaliação e Síntese de Substâncias Bioativas (LASSBio), Institute of Biomedical Sciences, Federal University of Rio de Janeiro (UFRJ), PO Box 68023, 21941-902 Rio de Janeiro, RJ, Brazil.

Bioorganic & Medicinal Chemistry Letters
|July 15, 2018
PubMed
Summary

N-acylhydrazone (NAH) scaffolds show great promise in drug discovery. This review assesses bioactive NAH motifs, highlighting their therapeutic potential and challenges for future drug development.

Keywords:
Clinical trialsDrug discoveryDrugsN-AcylhydrazonePreclinicalTherapeutics

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Area of Science:

  • Medicinal Chemistry
  • Drug Design

Background:

  • N-acylhydrazone (NAH) is a versatile scaffold with significant potential in drug design.
  • Numerous approved drugs and compounds in clinical trials demonstrate the therapeutic value of NAH motifs.

Purpose of the Study:

  • To provide a comprehensive assessment of bioactive NAH scaffolds in preclinical and clinical studies.
  • To discuss current and future challenges in NAH-based drug discovery and propose strategies to overcome them.

Main Methods:

  • Literature review of published preclinical and clinical studies on bioactive NAH scaffolds.
  • Analysis of therapeutic landscape and drug discovery challenges associated with NAH motifs.

Main Results:

  • NAH scaffolds are present in several approved drugs (e.g., nitrofurazone, dantrolene) and advanced clinical candidates (e.g., PAC-1, LASSBio-294).
  • NAH-based compounds exhibit diverse therapeutic applications.

Conclusions:

  • Bioactive NAH motifs represent a promising area for drug discovery.
  • Addressing challenges in NAH-based drug development is crucial for future therapeutic advancements.